1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. AZ-5104

AZ-5104 

Cat. No.: HY-B0793 Purity: 99.92%
Handling Instructions

AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively.

For research use only. We do not sell to patients.

AZ-5104 Chemical Structure

AZ-5104 Chemical Structure

CAS No. : 1421373-98-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
5 mg USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 80 In-stock
Estimated Time of Arrival: December 31
50 mg USD 275 In-stock
Estimated Time of Arrival: December 31
100 mg USD 370 In-stock
Estimated Time of Arrival: December 31
200 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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1 g   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively.

IC50 & Target[1]

EGFRL858R/T790M

1 nM (IC50)

EGFRL858R

1 nM (IC50)

EGFRL861Q

6 nM (IC50)

EGFR

25 nM (IC50)

ErbB4

7 nM (IC50)

EGFRExon 19 deletion/T790M

 

In Vitro

AZ-5104 inhibits EGFR phosphorylation with IC50s of 2, 1, 2, 53, and 33 nM in H1975 (EGFRL858R/T790M), PC-9VanR (EGFRExon 19 deletion/T790M), PC-9 (EGFRExon 19 deletion), H2073 (WT), and LOVO (WT), respectively. AZ5104 exhibits a reduced selectivity margin against wild-type EGFR when compared to AZD9291. AZ5104 display minimal off-target activity against other non-HER family kinases, but has the potential to target both HER2 and HER4 kinase activity[1].

In Vivo

The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice[1].

Molecular Weight

485.58

Formula

C₂₇H₃₁N₇O₂

CAS No.

1421373-98-9

SMILES

C=CC(NC1=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (57.66 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0594 mL 10.2970 mL 20.5939 mL
5 mM 0.4119 mL 2.0594 mL 4.1188 mL
10 mM 0.2059 mL 1.0297 mL 2.0594 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.15 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.15 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.15 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Cells were treated for 2 h with a dose-response of each drug (AZ-5104). Wild-type cells were stimulated for 10 minutes with 25 ng/mL of EGF before lysis. Level of EGFR phosphorylation was quantified in cell extracts using ELISA[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.92%

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Keywords:

AZ-5104AZ5104AZ 5104EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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